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Potent dihydroquinolinone dopamine D2 partial agonist/serotonin reuptake inhibitors for the treatment of schizophrenia
- Source :
- Bioorganicmedicinal chemistry letters. 20(9)
- Publication Year :
- 2010
-
Abstract
- A dihydroquinolinone moiety was found to be a potent serotonin reuptake inhibitor pharmacophore when combined with certain amines. This fragment was coupled with selected D2 ligands to prepare a series of dual acting compounds with attractive in vitro profiles as dopamine D2 partial agonists and serotonin reuptake inhibitors. Structure–activity studies revealed that the linker plays a key role in contributing to D2 affinity, function, and SRI activity.
- Subjects :
- Serotonin reuptake inhibitor
Clinical Biochemistry
Pharmaceutical Science
Pharmacology
Quinolones
Biochemistry
Partial agonist
Reuptake
Structure-Activity Relationship
Dopamine receptor D2
Drug Discovery
Moiety
Animals
Molecular Biology
biology
Chemistry
Receptors, Dopamine D2
Organic Chemistry
Disease Models, Animal
Norepinephrine transporter
Dopamine Agonists
Receptor, Serotonin, 5-HT1A
biology.protein
Schizophrenia
Molecular Medicine
Pharmacophore
Endogenous agonist
Selective Serotonin Reuptake Inhibitors
Antipsychotic Agents
Subjects
Details
- ISSN :
- 14643405
- Volume :
- 20
- Issue :
- 9
- Database :
- OpenAIRE
- Journal :
- Bioorganicmedicinal chemistry letters
- Accession number :
- edsair.doi.dedup.....5166982a958128acf3a0153c1b0e0b45